2. Academic Validation
  3. The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413

The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413

  • Int J Med Chem. 2011:2011:424535. doi: 10.1155/2011/424535.
Yvonne Connolly Martin 1
Affiliations

Affiliation

  • 1 Department of Global Pharmaceutical Research and Development, Martin Consulting, Waukegan, IL 60064, USA.
PMID: 25954518 DOI: 10.1155/2011/424535
Abstract

The novel selective D1 dopaminergic full agonists A-68930, A-77636 were discovered by the synthesis of molecules to probe the bioactive conformation of the partial agonist SKF-38393, by the use of this information to add D1 affinity and selectivity to a screening hit, and by traditional medicinal chemistry exploration of structure-activity relationships. The subsequent design of A-86929 and ABT-413 capitalized on these results, recently disclosed agonists, and traditional medicinal chemistry.

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